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[口服荨麻属植物提取物后健康受试者全血中的细胞因子分泌情况]

[Cytokine secretion in whole blood of healthy subjects following oral administration of Urtica dioica L. plant extract].

作者信息

Teucher T, Obertreis B, Ruttkowski T, Schmitz H

机构信息

Strathmann AG & Co., Hamburg.

出版信息

Arzneimittelforschung. 1996 Sep;46(9):906-10.

PMID:8967906
Abstract

Twenty healthy volunteers ingested for 21 days 2 capsules b.i.d. of an IDS 23/1 containing nettle leaf extract (Rheuma-Hek). Before and after 7 and 21 days the basal and the lipopolysaccharide (LPS) stimulated tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta) and interleukin-6 (IL-6) concentrations were measured ex vivo. In vitro the effects of IDS 23/1 on the release of these cytokines were determined. Additionally basal interleukin-4 (IL-4) and interleukin-10 (IL-10) levels were recorded. Orally taken the test drug has ex vivo no effect on basal levels of TNF-alpha, IL-1 beta, IL-4, IL-6 or IL-10 which were always below detection limits. After 7 and 21 days ingestion ex vivo a decrease of LPS stimulated TNF-alpha release of 14.6 and 24.0%, respectively, was observed. IL-1 beta was reduced for 19.2 and 39.3%. In vitro IDS 23/1 added to whole blood resulted in an exceeded inhibition of LPS stimulated TNF-alpha and IL-1 beta secretion which correlated with the duration of the drug ingestion. Using the highest tested IDS 23/1 concentration the inhibition reached 50.5 (day 0) to 79.5% (day 21) for TNF-alpha and 90.0 (day 0) to 99.2% (day 21) for IL-1 beta, respectively. IDS 23/1 induced a pronounced release of IL-6 in absence of LPS only in vitro. The detected IL-6 concentrations were comparable to those after LPS stimulation, additive effects could not be observed. The absence of detectable IL-6 concentrations in whole blood ex vivo after oral ingestion of the tested drug as well as the differences in the inhibition patterns for TNF-alpha and IL-1 beta ex vivo and ex vivo in vitro suggest that the extract contains different pharmacological effective compounds with varying bioavailabilities.

摘要

20名健康志愿者连续21天,每天两次,每次服用2粒含荨麻叶提取物(Rheuma - Hek)的IDS 23/1胶囊。在第7天和第21天前后,离体测定基础状态以及脂多糖(LPS)刺激后的肿瘤坏死因子-α(TNF-α)、白细胞介素-1β(IL-1β)和白细胞介素-6(IL-6)的浓度。在体外测定IDS 23/1对这些细胞因子释放的影响。此外,记录基础白细胞介素-4(IL-4)和白细胞介素-10(IL-10)水平。口服受试药物对TNF-α、IL-1β、IL-4、IL-6或IL-10的基础水平无离体影响,这些水平始终低于检测限。在摄入7天和21天后,离体观察到LPS刺激的TNF-α释放分别降低了14.6%和24.0%。IL-1β分别降低了19.2%和39.3%。在体外将IDS 23/1加入全血中,导致对LPS刺激的TNF-α和IL-1β分泌的抑制作用增强,这与药物摄入的持续时间相关。使用测试的最高IDS 23/1浓度时,对TNF-α的抑制率从第0天的50.5%达到第21天的79.5%,对IL-1β的抑制率从第0天的90.0%达到第21天的99.2%。仅在体外,IDS 23/1在无LPS的情况下诱导IL-6的显著释放。检测到的IL-6浓度与LPS刺激后的浓度相当,未观察到相加效应。口服受试药物后全血离体时未检测到IL-6浓度,以及TNF-α和IL-1β在离体和体外抑制模式的差异表明,该提取物含有具有不同生物利用度的不同药理活性化合物。

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